Antihistamines: generation after generation. Types of antihistamines and the range of their use Main antihistamines

To suppress the development of an allergic reaction, it is necessary to take an antihistamine. Currently, there are a huge number of medicines from this group. All of them are divided by generations. The list of new generation antihistamines is quite wide and allows you to choose the best medicine for treatment. In the article we will take a closer look at the most effective medicines in this category.

General concept

Most people have heard of antihistamines, but not everyone knows what they are and how they work. This is the name of a group of drugs that can act on histamine receptors, a mediator of allergic reactions. Upon contact with an irritant, the human body begins to produce specific substances, among which histamine is the most active. When this substance “meets” with certain receptors, symptoms such as tearing, reddening of the skin, itching, and a rash develop.

Antiallergic drugs are able to block these receptors and, as a result, resist the appearance of unpleasant symptoms. Without them, negative processes in the body will continue.

Currently, there is a significant increase in the number of people suffering from this or that type of allergy. An inadequate reaction of the immune system can develop against the background of disorders of the endocrine or nervous system, but most often the cause is external irritants: plant pollen, wool, dust, chemicals, some foods.

Treatment with antihistamines

In most cases, allergies cannot be completely cured. Medicines that affect histamine receptors will help get rid of unpleasant symptoms or prevent their occurrence.

To date, there are several generations of these medicines. And if the first antiallergic drugs brought not only long-awaited relief, but also many side effects, then the new generation antihistamines, the list of which we will consider below, are practically devoid of drawbacks and have practically no contraindications for use.

Medicines of this category are prescribed in the following cases:

  • with year-round or seasonal rhinitis;
  • with a negative reaction to flowering plants;
  • when symptoms of food and drug allergies occur;
  • with atopic dermatitis;
  • with urticaria and itching of the skin;
  • with bronchial asthma;
  • with angioedema;
  • with allergic conjunctivitis.

New generation antihistamines: an overview

Among all antiallergic medicines, the latest generation of drugs are considered the safest. They belong to prodrugs, which means that when they enter the body, the substances contained in the composition are converted into active metabolites. Such agents act only on histamine H-1 receptors and do not adversely affect the central nervous system.

The list of new generation antihistamines is small, however, compared with the precursor drugs, they can be prescribed to almost all patients suffering from various types of allergic reactions. Such funds allow you to quickly stop the already manifested symptoms and do not have a toxic effect on the heart. The following drugs are popular:

  • "Cetirizine".
  • "Fexofenadine".
  • "Erius".
  • "Fexofast".
  • "Ksizal".
  • "Levocetirizine".
  • "Desal".
  • "Caesera".
  • "Desloratadine".
  • "Kestin".

Features of drugs

The most common antiallergic drugs of the latest generation are those that contain fexofenadine in their composition. The substance belongs to selective inhibitors of H-1 histamine receptors and is able to stabilize mast cell membranes. The component inhibits the process of migration of leukocytes to the focus of the inflammatory process.

4th generation antihistamines based on cetirizine are considered one of the most effective. They are able to quickly stop the development of skin allergic reactions. They have a pronounced antipruritic and antiexudative effect.

Each of the modern anti-allergy drugs is prescribed only after the examination. The dosage regimen and duration of use is determined strictly individually.

"Erius": a description of the medication

An antihistamine based on desloratadine is produced by a branch of the pharmaceutical company Schering-Plough Corporation / USA in Belgium. You can buy medicines in tablet form and in the form of syrup. In addition to the main active ingredient, the tablets contain titanium dioxide, talc, calcium hydrogen phosphate dihydrate, lactose monohydrate, white wax, corn starch, microcrystalline cellulose.

The syrup contains such auxiliary components as citric acid, sorbitol, sodium benzoate, propylene glycol, sodium citrate dihydrate, sucrose. Tablets are packaged in packs of 7 and 10 pieces per blister. The syrup has the appearance of a yellow liquid and is available in 60 and 120 ml bottles.

Indications for appointment

Tablets "Erius" instructions for use recommend taking with seasonal rhinitis, lacrimation, itching of the nasal mucosa, seasonal pollinosis, chronic idiopathic urticaria. As prescribed by a specialist, the medication can also be used for other allergic conditions. For example, many patients say that "Erius" copes well with signs of neurodermatitis, food allergies, atopic dermatitis.

As part of complex therapy, an antihistamine can be taken for chicken pox, pink lichen, scabies and pseudo-scabies. "Erius" will effectively eliminate severe itching and help you fall asleep.

In pediatric practice, an antiallergic drug is used in the form of a syrup. The manufacturer claims that it can be given to babies older than 1 year. The dosage will depend on the age category. Erius tablets are suitable for adult patients and children from 12 years of age. Instructions for use recommends taking 1 tablet (5 mg) per day.

"Cetirizine": reviews

Modern antiallergic drugs are able to stop the development of the disease at the earliest stages. This is extremely important in severe allergic reactions. That is why many experts in the list of new generation antihistamines in the first place is "Cetirizine". An agent based on the active ingredient of the same name quickly relieves bronchospasm, attacks of bronchial asthma, and prevents the development of Quincke's edema. In addition, the medication will be effective for hives, pollinosis, hay fever, eczema, allergic dermatitis.

The antihistamine drug "Cetirizine" is available in the form of drops for oral administration, syrup and tablets. 1 ml of liquid solution contains 10 mg of cetirizine. One tablet contains the same amount of active substance. A noticeable effect from the use of a histamine H-1 receptor blocker can be seen an hour after administration. The duration of action is 24 hours. In bronchial asthma, it is used in combination with the bronchodilator drug Fenspiride.

Contraindications and side effects

Treatment with "Cetirizine" should be abandoned in case of hypersensitivity to the main component and hydroxyzine. It is forbidden to prescribe an antihistamine to people who are on hemodialysis or have kidney failure, during breastfeeding and pregnancy. Contraindications are also conditions associated with lactase deficiency, glucose-galactose malabsorption and lactose intolerance. With caution take "Cetirizine" simultaneously with barbiturates, ethanol-containing drugs and opioid analgesics.

Excellent tolerance is a huge advantage of the drug. Side effects while taking tablets, drops or syrup are extremely rare. This is mainly due to an overdose of the active substance. In such cases, the following symptoms may develop:

  • dizziness;
  • migraine;
  • nervous excitement;
  • tachycardia;
  • insomnia;
  • urinary retention;
  • myalgia;
  • skin rashes, eczema.

What is Kestin?

Another effective histamine receptor blocker is Kestin. It is produced by the pharmaceutical company Nycomed Danmark ApS (Denmark). Modern antiallergic agent is quite expensive. The average price of tablets (10 pieces per pack) is 380-400 rubles.

What is the composition of this medicine? Ebastine is the main component that blocks histamine H-1 receptors. The substance quickly eliminates spasms of the smooth muscles of the bronchi, reduces exudation, stops the manifestation of skin allergic reactions. "Kestin" is available in the form of tablets, which may contain various amounts of ebastine (10 or 20 mg) and syrup. The manufacturer also offers lozenges containing 20 mg of the active substance.

Who suits?

Any 4th generation antihistamines, including Kestin, can be taken only after consultation with an allergist. Most often, the drug is prescribed to adult patients. The instruction allows the use of tablets in pediatric practice, but only if the child is over 12 years old. Lozenges are prescribed only from the age of 15. The syrup can be used to treat children from 6 years of age.

"Kestin" effectively eliminates the symptoms of year-round and seasonal rhinitis of various origins, conjunctivitis, urticaria, Quincke's edema. The drug relieves symptoms caused by drug, food, insect allergies.

It is worth refraining from using "Kestin" during pregnancy, lactation, with intolerance to ebastine or other components of the drug. Lozenges are not prescribed for patients suffering from phenylketonuria. Under the supervision of a physician, an antihistamine is used for ischemic disease, hypokalemia, renal and hepatic insufficiency.

Description of the drug "Ksizal"

If necessary, symptomatic treatment of allergic skin reactions, urticaria, rhinorrhea, Quincke's edema, hay fever, many prefer the modern remedy "Ksizal". The cost of one package is 420-460 rubles. The drug is produced at pharmaceutical factories in Belgium, Switzerland and Italy.

The main active component of Xyzal is levocetirizine. The substance has pronounced anti-allergic properties. The active metabolite is able to prevent the development of allergies or significantly alleviate the course of the pathological condition. The substance reduces the permeability of the vascular walls, blocks the activity of cytokines and inflammatory mediators, and inhibits the movement of eosinophils. The clinical effect of the drug persists for 24 hours.

When are they assigned?

In the list of new allergy drugs, Xyzal occupies the first position due to its quick effect and safety. A modern drug has practically no contraindications to the appointment and rarely provokes the development of side effects. It is recommended to use it for a variety of allergic reactions: Quincke's edema, pollinosis, allergic dermatitis, itching, sneezing, nasal congestion against the background of seasonal or year-round rhinitis.

In the form of drops, "Ksizal" can be prescribed to babies from 2 years old. The tablets are suitable for use in children from 6 years of age and adults. The drug received many positive recommendations related to ease of use. One tablet of "Ksizal" can relieve allergy symptoms for a whole day.

"Levocetirizine" for allergies

The drug "Levocetirizine" is a cheaper analogue of "Ksizal". The cost of one package (10 tablets) ranges from 230-250 rubles. Also, the medicine can be purchased in the form of syrup and drops.

The active substance of the drug is able to block the endings of H-1 histamine receptors, thereby preventing the development of an inadequate response of the immune system. Allergy tablets "Levocetirizine" will be effective for hay fever, allergic dermatitis, seasonal and chronic rhinitis, lacrimation, sneezing, angioedema, urticaria.

The drug is not used to treat children under 6 years of age, during pregnancy and breastfeeding, with increased sensitivity to the components in the composition and severe renal failure.

The drug "Bamipin"

The list of new generation antihistamines includes agents intended for systemic use. However, in some cases, local medication is also required. To cope with skin manifestations of allergies, you should use special gels. One of these external medicines is Bamipin. It can be used already with the appearance of the first symptoms of urticaria, an allergic reaction to insect bites, itching of the skin, thermal burns. The drug is also available in the form of tablets.

1st generation antihistamines

According to their chemical structure, these drugs are divided into the following groups:

    1) derivatives of aminoalkyl ethers - diphenhydramine (diphenhydramine, benadryl, alphadryl), amidryl, etc.
    2) ethylenediamine derivatives - antergan (suprastin), allergan, dehistine, mepyramine, etc.
    3) derivatives of phenothiazines - promethazine (pipolphen, diprazine, phenergan), doxergan, etc.
    4) derivatives of alkylamines - pheniramine (trimeton), triprolidine (actadil), dimetindine (fenostil), etc.
    5) derivatives of benzhydryl ethers - clemastine (tavegil).
    6) piperidine derivatives - cyproheptadine (peritol), cyprodine, astonine, etc.
    7) quinuclidine derivatives - quifenadine (fencarol), sequifenadine (bicarfen).
    8) piperazine derivatives - cyclizine, meclizine, chlorcyclizine, etc.
    9) alphacarboline derivatives - diazolin (omeril).
Diphenhydramine(diphenhydramine, alfadril, etc.) has a fairly high antihistamine activity, has a local anesthetic effect (numbness of the mucous membranes), reduces smooth muscle spasm, has lipophilicity and penetrates the blood-brain barrier, therefore it has a pronounced sedative effect, similar to the action of neuroleptic drugs, in large doses has a hypnotic effect. This drug and its analogues inhibit the conduction of nervous excitation in the autonomic ganglia and have a central anticholinergic effect, therefore they increase the dryness of the mucous membranes and the viscosity of secretions, can cause agitation, headache, trembling, dry mouth, urinary retention, tachycardia, constipation. Assigned inside 2-3 times a day, intramuscularly.

Suprastin(chloropyramine) has a pronounced antihistamine and M-anticholinergic effect, penetrates the blood-brain barrier, causes drowsiness, general weakness, dry mucous membranes and increases the viscosity of secretions, irritation of the gastrointestinal mucosa, headache, dry mouth, urinary retention, tachycardia, glaucoma. Assigned inside 2-3 times a day, intramuscularly.

Promethazine(pipolfen, diprazine) has a strong antihistamine activity, is well absorbed and easily penetrates the blood-brain barrier with different routes of administration, and therefore has a significant sedative activity, enhances the effect of narcotic, hypnotic, analgesic and local anesthetics, lowers body temperature, prevents and soothes vomiting. It has a moderate central and peripheral anticholinergic effect. When administered intravenously, it can cause a drop in systemic arterial pressure, collapse. They are administered orally and intramuscularly.

clemastine(tavegil) is one of the most common and effective antihistamines of the 1st generation, it selectively and actively blocks H1 receptors, acts longer (8-12 hours), poorly penetrates the blood-brain barrier, therefore it does not have sedative activity and does not causes a drop in blood pressure. It is recommended for use in acute allergic reactions parenterally (anaphylactic shock, severe forms of allergic dermatosis).

Diazolin(omeril) has less antihistamine activity, but practically does not penetrate the blood-brain barrier and does not cause sedative and hypnotic effects, it is well tolerated.

Fenkarol(quifenadine) is an original antihistamine drug that moderately blocks H1 receptors and reduces the content of histamine in tissues, has a low lipophilicity, does not penetrate the blood-brain barrier and does not have sedative and hypnotic effects, does not have adrenolytic and anticholinergic activity, has an antiarrhythmic effect. Children under the age of 3 years are prescribed 0.005 g, from 3 to 12 years old - 0.01 g each, over 12 years old - 0.025 g 2-3 times a day.

Peritol(cyproheptadine) moderately blocks H1 receptors, has a strong antiserotonin activity, as well as an M-anticholinergic effect, penetrates the blood-brain barrier and has a pronounced sedative effect, reduces the hypersecretion of ACTH and somatotropin, increases appetite, and reduces the secretion of gastric juice. It is prescribed for children from 2 to 6 years old - 6 mg in three doses, over 6 years old - 4 mg 3 times a day.

Comparative characteristics of the most common antihistamines of the 1st generation are presented in Table. 3.

Table 3 1st generation antihistamines recommended for the treatment of allergic pathology in children

Options / ActionsDiphenhydramineTavegilSuprastinFenkarolDiazolinPeritolPipolfen
Sedation ++ +/- + -- -- - +++
M-cholinergic. Effect + + + -- + +/- +
Start of action 2 hours2 hours2 hours2 hours2 hours2 hours20 minutes.
Half-life 4-6 hours1-2 hours6-8 hours4-6 hours6-8 hours4-6 hours8-12 hours
Frequency of administration per day 3-4 times2 times2-3 times3-4 times1-3 times3-4 times2-3 times
Application time after mealafter mealwhile eatingafter mealafter mealafter mealafter meal
Interaction with other drugs enhances the action of hypnotics, neuroleptics, anticonvulsantsenhances the effect of hypnotics and MAO inhibitorsmoderately enhances the effect of hypnotics and neurolepticslowers the content of histamine in tissues, has an anti-arrhythmic effect - has an anti-serotonin effect, reduces the secretion of ACTHenhances the effect of narcotic, hypnotic, local anesthetics
Side effects agitation, drop in blood pressure, dry mouth, difficulty breathingnot prescribed before 1 year, bronchospasm, urinary obstruction, constipationdry mouth, increased levels of transaminases, irritation of the gastric mucosa and 12-finger. gutsdry mouth, sometimes nauseadry mouth, irritation of the mucous membrane of the stomach and 12-finger. gutsdry mouth, drowsiness, nauseashort-term drop in blood pressure, increased levels of transaminases, photosensitizing effect

Features of the pharmacological effects of 1st generation antihistamines

As shown in Table. 3, antihistamines of the first generation, by noncompetitively and reversibly inhibiting H1 receptors, block other receptor formations, in particular, cholinergic muscarinic receptors and thus have an M1 cholinergic effect. Their atropine-like action can cause dry mucous membranes and exacerbate bronchial obstruction. To achieve a pronounced antihistamine effect, high concentrations of these drugs in the blood are required, which requires the appointment of large doses. In addition, these compounds act quickly after administration, but for a short time, which requires their repeated use (4-6 times) during the day. It is important to note that antihistamines have an effect on the central nervous system, penetrating the blood-brain barrier, and can cause blockade of H1 receptors in cells of the central nervous system, which causes their undesirable sedative effect.

The most important property of these drugs, which determines the ease of penetration through the blood-brain barrier, is their lipophilicity. The sedative effects of these drugs, ranging from mild drowsiness to deep sleep, can often occur even at their usual therapeutic doses. Essentially, all 1st generation antihistamines have a pronounced sedative effect to one degree or another, most noticeable in phenothiazines (pipolphen), ethanolamines (diphenhydramine), piperidines (peritol), ethylenediamines (suprastin), to a lesser extent - in alkylamines and benzhydryl ether derivatives (clemastine, tavegil). The sedative effect is practically absent in quinuclidine derivatives (fencarol).

Another undesirable manifestation of the action of these drugs on the central nervous system is coordination disorders, dizziness, a feeling of lethargy, and a decrease in the ability to concentrate. Some 1st generation antihistamines exhibit the properties of local anesthetics, have the ability to stabilize biomembranes and, by prolonging the refractory phase, can cause cardiac arrhythmias. Some drugs of this group (pipolfen), potentiating the effects of catecholamines, cause fluctuations in blood pressure (Table 3).

Among the undesirable effects of these drugs, it should also be noted an increase in appetite, most pronounced in piperidines (peritol) and the occurrence of functional disorders of the gastrointestinal tract (nausea, vomiting, discomfort in the epigastric region), more often manifested when taking ethylenediamines (suprastin, diazolin). For most 1st generation antihistamines, peak concentrations are reached after 2 hours. However, a negative characteristic of H1-antagonists of the 1st generation is the rather frequent development of tachyphylaxis - a decrease in therapeutic efficacy during their long-term use (Table 4).

Table 4 Unwanted side effects of first generation antihistamines:

  • 1. Pronounced sedative and hypnotic effect
  • 2. Negative effect on the central nervous system - impaired coordination, dizziness, decreased concentration
  • 3. M-cholinergic (atropine-like) action
  • 4. Development of tachyphylaxis
  • 5. Short duration of action and repeated use
Due to the peculiarities of the pharmacological action of the 1st generation antihistamines, certain restrictions on their use have now been established (Table 5). Therefore, in order to prevent tachyphylaxis, when prescribing these drugs, they should be alternated every 7-10 days.

Table 5 Limitations of the clinical use of first-generation antihistamines:

  • astheno-depressive syndrome;
  • bronchial asthma, glaucoma;
  • spastic phenomena in the pyloric or duodenal areas;
  • atony of the intestines and bladder;
  • all activities that require active attention and quick response
Thus, the undesirable effects of 1st generation antihistamines limit their use in medical practice, especially in recent years. However, the relatively low cost of these drugs and the rapid action make it possible to recommend these drugs for the treatment of the acute period of allergic diseases in children in a short course (7 days). In the acute period, and especially in severe forms of allergic dermatosis in children, when parenteral administration of antihistamines is required, and taking into account the fact that there are no such 2nd generation drugs so far, tavegil is the most effective, which lasts longer (8-12 hours) , has a slight sedative effect and does not cause a drop in blood pressure. In anaphylactic shock, tavegil is also the drug of choice. Less effective in such cases is suprastin. In the subacute course of allergic dermatoses and especially in their itchy forms (atopic dermatitis, acute and chronic urticaria). in children with astheno-depressive syndrome, 1st generation antihistamines, mainly without sedation, can be used - phencarol and diazolin, which should be prescribed in a short course - 7-10 days. In allergic rhinitis (seasonal and year-round) and hay fever, the use of 1st generation antihistamines is undesirable, since they, having an M-cholinergic effect, can cause dry mucous membranes, increase the viscosity of the secretion and contribute to the development of sinusitis and sinusitis, and in bronchial asthma - cause or exacerbate bronchospasm. Due to the pronounced cardiovascular effect, the use of pipolfen in various forms of allergic diseases is currently very limited.

2nd generation antihistamines

Antihistamines of the 2nd generation have been widely used in allergological practice in recent years. These drugs have a number of advantages over 1st generation drugs (Table 6)

Table 6 Effects of second generation antihistamines

  • 1. Have very high specificity and affinity for H1 receptors
  • 2. Do not cause blockade of other types of receptors
  • 3. Do not have M-anticholinergic action
  • 4. In therapeutic doses, they do not penetrate the blood-brain barrier, do not have sedative and hypnotic effects
  • 5. They have a fast onset of action and a pronounced duration of the main effect (up to 24 hours)
  • 6. Well absorbed from the gastrointestinal tract
  • 7. No relationship has been established between drug absorption and food intake
  • 8. Can be applied at any time
  • 9. Do not cause tachyphylaxis
  • 10. Easy to use (1 time per day)
Obviously, these drugs meet the basic requirements for ideal antihistamines, which should be fast to show effect, long-acting (up to 24 hours) and be safe for patients. These requirements are largely met by 2nd generation antihistamines: claritin (loratadine), zyrtec (cetirizine), kestin (ebastine) (Table 7).

Table 7 2nd generation antihistamines recommended for the treatment of allergic pathology in children

Options
actions
Terfenadine
(terfen)
Astemizol
(hismanal)
Claritin
(loratadine)
Zyrtec
(cytirizine)
Kestin
(ebastine)
SedationNomay beNomay beNo
M-cholinergic. Effectthere isthere isNoNoNo
Start of action1-3 hours2-5 days30 minutes30 minutes30 minutes
Half-life4-6 hours8-10 days12-20 hours7-9 hours24 hours
Frequency of administration per day1-2 times1-2 times1 time1 time1 time
Connect with foodNoYesNoNoNo
Application timeanytime, preferably on an empty stomachon an empty stomach or 1 hour before mealsAnytimein the 2nd half of the day, better before bedAnytime
Pharmacological incompatibility with other drugsErythromycin, oleandomycin, clarithromycin, mycosolone Erythromycin, kenolone
Side effectsVentricular arrhythmias, QT prolongation, bradycardia, syncope, bronchospasm, hypokalemia, hypomagnesemia, increased transaminase activityVentricular arrhythmias, bradycardia, syncope, bronchospasm, increased transaminase activity, not indicated for children under 12 years of ageDry mouth (rare)Dry mouth (sometimes)Dry mouth (rare), abdominal pain (rare)
Efficiency at
atopic dermatitis:+/- +/- ++ ++ ++
with urticaria+/- +/- +++ ++ +++
Weight gainNoup to 5-8 kg in 2 monthsNoNoNo

Claritin (loratadine) is the most common antihistamine drug, it has a specific blocking effect on H1 receptors, for which it has a very high affinity, does not have anticholinergic activity and therefore does not cause dry mucous membranes and bronchospasm.

Claritin quickly acts on both phases of the allergic reaction, inhibits the production of a large number of cytokines, directly inhibits the expression of cell adhesion molecules (ICAM-1, VCAM-1, LFA-3, P-selectins and E-selectins), reduces the formation of leukotriene C4, thromboxane A2 , factors of eosinophil chemotaxis and platelet activation. Thus, claritin effectively prevents the formation of allergic inflammation and has a pronounced antiallergic effect (Leung D., 1997). These properties of claritin were the basis for its use as a basic remedy in the treatment of such allergic diseases as allergic rhinitis, conjunctivitis and hay fever.

Claritin also helps to reduce bronchial hyperreactivity, increases forced expiratory volume (FEV1) and peak expiratory flow, which determines its beneficial effect in bronchial asthma in children.

Claritin is effective and can currently be used as an alternative anti-inflammatory therapy, especially in mild persistent asthma, as well as in the so-called cough variant of bronchial asthma. In addition, this drug does not penetrate the blood-brain barrier, does not affect the activity of the NCS and does not potentiate the action of sedatives and alcohol. The sedative effect of claritin is not more than 4%, that is, it is detected at the placebo level.

Claritin does not have a negative effect on the cardiovascular system, even at concentrations exceeding the therapeutic dose by 16 times. Apparently, this is determined by the presence of several pathways of its metabolism (the main pathway is through the oxygenase activity of the CYP3A4 isoenzyme of the cytochrome P-450 system and the alternative pathway is through the CYP2D6 isoenzyme), therefore, claritin is compatible with macrolides and antifungal drugs imidazole derivatives (ketoconazole, etc.) , as well as with a number of other medicines, which is crucial when using these medicines simultaneously.

Claritin is available in tablets of 10 mg and in syrup, 5 ml of which contains 5 mg of the drug.

Claritin tablets are prescribed for children from the age of 2 years in the appropriate age dosage. The maximum plasma level of the drug is reached within 1 hour after ingestion, which ensures a rapid onset of effect. Food intake, impaired liver and kidney function do not affect the pharmacokinetics of claritin. The release of claritin occurs after 24 hours, which allows you to take it 1 time per day. Long-term use of Claritin does not cause tachyphylaxis and addiction, which is especially important in the treatment of itchy forms of allergic dermatosis (atopic dermatitis, acute and chronic urticaria and strophulus) in children. The effectiveness of claritin was studied by us in 147 patients with various forms of allergic dermatoses with a good therapeutic effect in 88.4% of cases. The best effect was obtained in the treatment of acute and especially chronic urticaria (92.2%), as well as atopic dermatitis and strophulus (76.5%). Given the high efficacy of claritin in the treatment of allergic dermatosis and its ability to inhibit the production of leukotrienes, we studied its effect on the activity of eicosanoid biosynthesis by peripheral blood granulocytes in patients with atopic dermatitis. The biosynthesis of prostanoids by peripheral blood leukocytes was studied by the radioisotope method using labeled arachidonic acid under in vitro conditions.

During treatment with claritin in patients with atopic dermatitis, a decrease in the biosynthesis of the studied eicosanoids was found. At the same time, the biosynthesis of PgE2 decreased most significantly - by 54.4%. The production of PgF2a, TxB2 and LTV4 decreased by an average of 30.3%, and prostacyclin biosynthesis decreased by 17.2% compared with the level before treatment. These data indicate a significant effect of claritin on the mechanisms of atopic dermatitis formation in children. It is obvious that the decrease in the formation of pro-inflammatory PTV4 and pro-aggregate TxB2 against the background of relatively unchanged prostacyclin biosynthesis is an important contribution of claritin to the normalization of microcirculation and the reduction of inflammation in the treatment of atopic dermatitis. Therefore, the revealed regularities of the effects of claritin on the mediator functions of eicosanoids should be taken into account in the complex therapy of allergic dermatoses in children. Our data allow us to conclude that the appointment of claritin is especially appropriate for allergic skin diseases in children. With dermorespiratory syndrome in children, claritin is also an effective drug, as it can simultaneously affect the skin and respiratory manifestations of allergies. The use of claritin in dermorespiratory syndrome for 6-8 weeks helps to improve the course of atopic dermatitis, reduce asthma symptoms, optimize external respiration, reduce bronchial hyperreactivity and reduce symptoms of allergic rhinitis.

Zyrtec(Cetirizine) is a pharmacologically active non-metabolizable product that has a specific blocking effect on H1 receptors. The drug has a pronounced antiallergic effect, as it inhibits the histamine-dependent (early) phase of the allergic reaction, reduces the migration of inflammatory cells and inhibits the release of mediators involved in the late phase of the allergic reaction.

Zyrtec reduces the hyperreactivity of the bronchial tree, does not have an M-anticholinergic effect, therefore it is widely used in the treatment of allergic rhinitis, conjunctivitis, pollinosis, as well as in their combination with bronchial asthma. The drug does not adversely affect the heart.

Zyrtec is available in tablets of 10 mg and in drops (1 ml = 20 drops = 10 mg), characterized by the rapid onset of the clinical effect and prolonged action due to its insignificant metabolism. It is prescribed for children from the age of two: from 2 to 6 years old, 0.5 tablets or 10 drops 1-2 times a day, for children 6-12 years old - 1 tablet or 20 drops 1-2 times a day.

The drug does not cause tachyphylaxis and can be used for a long time, which is important in the treatment of allergic skin lesions in children. Despite the indications of the absence of a pronounced sedative effect when taking Zyrtec, in 18.3% of observations we found that the drug, even at therapeutic doses, caused a sedative effect. In this regard, caution should be exercised when using Zirtek with sedatives because of the possible potentiation of their action, as well as in the pathology of the liver and kidneys. A positive therapeutic effect of the use of Zirtek was obtained by us in 83.2% of cases of treatment of allergic dermatoses in children. This effect was especially pronounced in itching forms of allergic dermatoses.

Kestin(Ebastine) has a pronounced selective H1-blocking effect, without causing anticholinergic and sedative effects, is rapidly absorbed and almost completely metabolized in the liver and intestines, turning into the active metabolite carebastin. Taking kestin with fatty foods increases its absorption and the formation of carebastin by 50%, which, however, does not affect the clinical effect. The drug is available in tablets of 10 mg and is used in children over 12 years of age. A pronounced antihistamine effect occurs 1 hour after ingestion and lasts 48 hours.

Kestin is effective in the treatment of allergic rhinitis, conjunctivitis, pollinosis, as well as in the complex therapy of various forms of allergic dermatosis - especially chronic recurrent urticaria and atopic dermatitis.

Kestin does not cause tachyphylaxis and can be used for a long time. At the same time, it is not recommended to exceed its therapeutic doses and be careful when prescribing ketin in combination with macrolides and some antifungal drugs, since it can cause a cardiotoxic effect. Despite the spread of such 2nd generation drugs as terfenadine and astemizole, we do not recommend their use in the treatment of allergic diseases in children, since some time after the start of using these drugs (since 1986), clinical and pharmacological data appeared, indicating the damaging effect of these drugs on the cardiovascular system and liver (cardiac arrhythmias, prolongation of the Q-T interval, bradycardia, hepatotoxicity). Mortality was established in 20% of patients treated with these drugs. Therefore, these drugs should be used with caution, not exceeding the therapeutic dose and not used in patients with hypokalemia, cardiac arrhythmias, congenital prolongation of the QT interval, and especially in combination with macrolides and antifungal drugs.

Thus, in recent years, the pharmacotherapy of allergic diseases in children has been replenished with a new group of effective H1 receptor antagonists, devoid of a number of negative properties of first-generation drugs. According to modern ideas, an ideal antihistamine drug should quickly show an effect, act for a long time (up to 24 hours) and be safe for patients. The choice of such a drug should be carried out taking into account the individuality of the patient and the characteristics of the clinical manifestations of allergic pathology, as well as taking into account the laws of the pharmacokinetics of the drug. Along with this, when assessing the priority of prescribing modern H1 receptor antagonists, special attention should be paid to the clinical efficacy and safety of such drugs for the patient. The selection criteria for second generation antihistamines are shown in Table 8.

Table 8 Criteria for choosing second-generation antihistamines

ClaritinZyrtecAstemizolTerfenadineKestin
Clinical Efficiency
Perennial allergic rhinitis++ ++ ++ ++ ++
Seasonal+++ +++ +++ +++ +++
Atopic dermatitis++ ++ ++ ++ ++
Hives+++ +++ +++ +++ +++
Strofulus+++ +++ +++ +++ +++
Toxidermia+++ +++ +++ +++ +++
Safety
SedationNoYesNoNoNo
Strengthening the effect of sedativesNoYesNoNoNo
Cardiotoxic effect: Q-T prolongation, hypokalemiaNoNoYesYesat a dose of more than 20 mg
Co-administration with macrolides and some antifungal drugsdoes not cause side effectsdoes not cause side effectscardiotoxic effectcardiotoxic effectin a dose of more than 20 mg, an effect on blood circulation is possible
Interaction with foodNoNoYesNoNo
Anticholinergic actionNoNoNoNoNo

Our studies and clinical observations indicate that such a second-generation antihistamine that satisfies the above conditions, is clinically effective and safe in the treatment of allergic diseases in children, is primarily claritin, and then - zyrtec.

According to medical statistics, the number of allergic reactions is steadily growing - this is associated with the constant deterioration of the environmental situation and a decrease in immunity in the conditions of civilization.

Suprastin perfectly relieves itching, accelerates the process of getting rid of skin rashes. This drug is approved for the treatment of infants (from 30 days of age), but the dosage must be selected on a strictly individual basis - the doctor will take into account the age and weight of the baby.

The antihistamine in question is used as a component of complex therapy against chickenpox (relieves itching), is part of the "troychatka" - a substance used to reduce body temperature.

Note:Suprastin is categorically contraindicated for use by pregnant women and women who are in the lactation period.

Tavegil

It is used in the same cases as suprastin. It has a long antihistamine effect - the effect persists for 12 hours. Tavegil does not cause a decrease in blood pressure, and its hypnotic effect is less pronounced than that of Suprastin.

In childhood, the drug in question is used from the age of 1 - babies are prescribed syrup, and children over 6 years old can also use tablets. The dosage is selected by the attending physician, taking into account the age and weight of the patient.

note:Tavegil is strictly prohibited for use during pregnancy.

Fenkarol

From this drug, the antihistamine effect is longer, since it not only blocks histamine receptors, but also triggers a specific enzyme that is able to utilize histamine. Fenkarol does not cause a hypnotic and sedative effect, it can be used as an antiarrhythmic agent.

The considered antiallergic drug is used to treat all types of allergies, it is especially valuable in the treatment. Fencarol is part of the complex therapy for parkinsonism, it is also used in surgery - they are given medical preparation for anesthesia.

In childhood, this drug is prescribed from 12 months, it is advisable to give babies a suspension that has an orange flavor. The dosage and duration of taking the drug is determined by the attending physician.

Note:Fenkarol is categorically contraindicated in the first trimester of pregnancy, and in the second and third trimesters it can be used to treat allergies only under the supervision of a specialist.

Fenistil

This drug is used to treat:

  • all types of allergies;
  • (relieves itching);

Fenistil causes drowsiness only at the very beginning of treatment, literally after a few days the sedative effect disappears. Fenistil has several side effects:

  • severe dryness of the oral mucosa;
  • muscle spasms.

This remedy is produced in the form of tablets, drops for children, gel and cream. The latest pharmacological forms of Fenistil are used for insect bites, and.

For children, Fenistil is prescribed from the age of one month in the form of drops, if the patient is older than 12 years, then tablets are prescribed to him.

Note:during pregnancy, Fenistil can be used in the form of a gel and drops, from the second trimester such appointments can only take place if there are conditions that threaten the woman's life - Quincke's edema, acute food allergies.

Diazolin

It has a low antihistamine activity, but it has a lot of side effects:

  • dizziness;
  • cardiopalmus;
  • frequent urination.

Diazolin also has a certain advantage - it does not cause drowsiness, therefore it can be prescribed to treat an allergic reaction in pilots and drivers. The duration of the antiallergic action of the drug in question is a maximum of 8 hours.

Diazolin can be prescribed for children from 2 years old, up to 5 years it is better to give children the drug in the form of a suspension, older ones can also be offered tablets.

Note:Diazolin is categorically contraindicated in the first trimester of pregnancy.

Despite the fact that first-generation antihistamines have a lot of drawbacks, they are actively used in medical practice: each remedy is well studied, in most cases they are approved for use by children.

Second generation antihistamines

They are called non-sedative, have a pronounced antihistamine effect, the duration of which often reaches 24 hours. Such drugs are taken 1 time per day, do not cause drowsiness and impaired attention.

Most often, these funds are used to treat eczema, urticaria, Quincke's edema and hay fever. Often, second-generation antihistamines are used in treatment - they perfectly relieve itching. A distinctive advantage of this group of drugs is that they are not addictive. There is also a nuance in the use of second-generation antiallergic drugs - they are not recommended for the elderly and those who have a history of heart disease.

Loratadine

The drug acts selectively on histamine receptors, which allows you to achieve a quick effect. Produced in the form of tablets and syrup, it can be sold under the name "Claritin" or "Lomilan". The syrup is very easy to dose and give to children, and the effect of the drug begins to appear within an hour after consumption.

In childhood, Loratadine is prescribed from the age of 2, the dosage and duration of administration should be selected only by the attending physician.

Note:the antihistamine in question is not recommended for pregnant women in the early stages (up to 12 weeks). In extreme cases, the use of Loratadine must be carried out under the supervision of a specialist.

Kestin

The drug has a number of pronounced advantages:

  • selectively blocks histamine receptors;
  • does not cause drowsiness;
  • the effect is noticeable within an hour after use;
  • antiallergic effect persists for 48 hours.

In pediatric practice, Kestin has been used since the age of 12, but it can have a toxic effect on the liver and reduce heart rate.

Kestin is absolutely contraindicated during pregnancy.

Rupafin

The drug is most often used for treatment, after ingestion it is rapidly absorbed, and the simultaneous intake of food greatly enhances the effect of Rupafin.

The medicinal product in question is not used for children under 12 years of age and pregnant women. If the use of the drug in children who are breastfed is required, then this is possible only under strict medical supervision.

Antihistamines of the second generation fully meet the modern requirements for medicines - they are highly effective, have a long-lasting effect, and are easy to use. It should be remembered that such drugs should be used in a strictly prescribed dosage, because its excess leads to drowsiness and increased side effects.

Third generation antihistamines

It is worth mentioning right away that you can find the division of antihistamines into the third and fourth generation - it is very conditional and carries nothing but a beautiful, effective marketing slogan.

Antihistamines of the third generation are among the most modern, they do not have a sedative effect, they do not affect the functioning of the heart. Such funds are actively used to treat all types of allergies, dermatitis, even in children and people with a history of cardiac pathologies.

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Allegra, Cetirizine, Xizal and Desloratadine - these drugs belong to the third generation antiallergic drugs. All these funds should be used with extreme caution by pregnant women - for the most part they are contraindicated. In addition, the prescribed dosage must be strictly observed, since its excess can result in headaches, dizziness and too frequent heartbeats.

Antihistamines should be prescribed by a doctor, he will also select the dosage, give recommendations on the duration of the course of treatment. If the patient violates the treatment regimen, then this can provoke not only the appearance of side effects, but also an increase in the allergic reaction.

Tsygankova Yana Alexandrovna, medical observer, therapist of the highest qualification category

Every year the number of allergic reactions, including dermatitis, is steadily growing, which is associated with the deterioration of the environmental situation and the "unloading" of the immune system in the conditions of civilization.

Allergy is a hypersensitivity reaction of the body to a foreign chemical substance - an allergen. It can be food, pet hair, dust, drugs, bacteria, viruses, vaccines, and more.

In response to the entry of an allergen in the organs and cells of the immune system, an intensive production of a special substance, histamine, begins. This substance binds to H1 - histamine receptors and causes signs of allergy.

If you remove the provoking factor, the manifestations of allergies will pass over time, but the cells that store the memory of this substance will remain in the blood. At the next meeting with him, an allergic reaction may manifest itself with greater force.

How do antihistamines work?

These drugs bind to H1-histamine receptors and block them. Thus, histamine cannot bind to the receptors. Allergy phenomena subside: the rash turns pale, swelling and itching of the skin decrease, nasal breathing is facilitated and the phenomena of conjunctivitis decrease.

The first antihistamine drugs appeared in the 1930s. As science and medicine developed, the second and then the third generation of antihistamines were created. All three generations are used in medicine. The list of antihistamines is constantly updated. Analogues are produced, new forms of release appear.

Consider the most popular drugs, starting with the latest generation.

In fairness, the division into the first, second and third generations makes sense, because. substances differ in properties and side effects.

The division into the third and fourth generation is very conditional, and often carries nothing but a beautiful marketing slogan.

Sometimes these drugs are referred to both the third and fourth generations at the same time. We will not confuse you even more and call it all simpler:

Last generation - metabolites

The most modern medicines rstva. A distinctive feature of this generation is that the drugs are prodrugs. When ingested, they are metabolized - activated in the liver. Do drugs no sedative effect, also they do not affect the functioning of the heart.

Antihistamines of the new generation are successfully used to treat all types of allergies and allergic varieties of dermatitis in children, people suffering from cardiovascular diseases. Also, these funds are prescribed to people whose profession is associated with increased attention (drivers, surgeons, pilots).

Allegra (Telfast)

The active substance is fexofenadine. The drug not only blocks histamine receptors, but also reduces its production. It is used for chronic urticaria and seasonal allergies. The anti-allergic effect lasts up to 24 hours after the end of the course of treatment. Not addictive.

Available only in the form of tablets. Previously, the tablets were called Telfast, now - Allegra. They are contraindicated in children under 12 years of age, pregnant and lactating women.

cetirizine

The effect after administration develops after 20 minutes and persists for 3 days after discontinuation of the drug. It is used to treat and prevent allergies. Cetirizine does not cause drowsiness and decreased attention. It may be used for a long time. The drug is available in the form of drops (trade name "Zirtek", "Zodak"), syrup ("Cetrin", "Zodak") and tablets.

In children's practice, it is used from 6 months in the form of drops, from 1 year in the form of syrup. From the age of 6, tablets are allowed. The dosage is determined by the doctor individually.

Pregnant women Cetirizine is strictly contraindicated. For the period of use, it is desirable to stop breastfeeding.

The medicine is prescribed for the treatment of year-round and seasonal allergies, urticaria and pruritus. The action occurs 40 minutes after administration. Available in the form of drops and tablets.

In children's practice, drops are used from the age of 2 and tablets from the age of 6. The dosage is determined by the doctor in accordance with the weight and age of the child.

The drug is contraindicated for pregnant women. Acceptance during breastfeeding is allowed.

Desloratadine

Synonyms: Lordestin, Desal, Erius.

The drug has an antihistamine and anti-inflammatory effect. Well eliminates the signs of seasonal allergies and chronic urticaria. When taken in therapeutic doses, dry mouth and headache may occur. Available in the form of syrup, tablets.

Children are prescribed from 2 years in the form of syrup. Tablets are allowed for children over 6 years of age.

Pregnant and lactating Desloratadine is contraindicated. Perhaps its use in life-threatening conditions: Quincke's edema, suffocation (bronchospasm).

Antihistamines of the 3rd generation effectively eliminate the manifestations of allergies. In therapeutic doses, they do not cause drowsiness and reduce attention. However, if the recommended dosages are exceeded, dizziness, headache, and an increase in heart rate may occur.

If you have used any of their preparations, do not forget to leave a review in the comments.

Second generation - non-sedating

The drugs of this group have a pronounced antihistamine effect, the duration of which is up to 24 hours. This allows you to take them 1 time per day. Medications do not cause drowsiness or impaired attention, which is why they are called non-sedating.

Non-sedative drugs are actively used to treat:

  • urticaria;
  • hay fever;
  • eczema;

These remedies are also used to relieve severe itching in chickenpox. There is no addiction to antiallergic drugs of the 2nd generation. They are quickly absorbed from the digestive tract. They can be taken at any time, even with meals.

Loratadine

The active substance is loratadine. The drug selectively affects H1 histamine receptors, which allows you to quickly eliminate allergies and reduce the number of side effects:

  • anxiety, sleep disturbances, depression;
  • frequent urination;
  • constipation;
  • asthma attacks are possible;
  • increase in body weight.

Produced in the form of tablets and syrup (trade names "Claritin", "Lomilan"). Syrup (suspension) is convenient to dose and give to young children. The action develops 1 hour after administration.

In children, Loratadine is used from the age of 2 years in the form of a suspension. The dosage is selected by the doctor depending on the body weight and age of the child.

Loratadine is prohibited for use in the first 12 weeks of pregnancy. In extreme cases, it is prescribed under the strict supervision of a physician.

Synonym: Ebastine

This agent selectively blocks H1 histamine receptors. Does not cause drowsiness. The action occurs 1 hour after administration. The antihistamine effect persists for 48 hours.

In children, it is used from 12 years of age. Kestin has a toxic effect on the liver, causes rhythm disturbances, and reduces the heart rate. Pregnant women are contraindicated.

Synonym: Rupatadin

The medicine is used in the treatment of hives. After oral administration, it is rapidly absorbed. Simultaneous food intake enhances the effect of Rupafin. It is not used in children under 12 and pregnant women. Use during breastfeeding is possible only under strict medical supervision.

Antihistamines of the 2nd generation meet all modern requirements for medicines: high efficiency, safety, long-term effect, ease of use.

However, it should be remembered that exceeding the therapeutic dosage leads to the opposite effect: drowsiness appears and side effects increase.

First generation - sedatives

Sedative drugs are called because they cause a sedative, hypnotic, mind-depressing effect. Each representative of this group has a sedative effect expressed to varying degrees.

In addition, the first generation of drugs has a short-term anti-allergic effect - from 4 to 8 hours. They may become addictive.

However, the drugs are time-tested and often inexpensive. This explains their mass.

First-generation antihistamines are prescribed to treat allergic reactions, relieve skin itching in infectious rashes, to reduce the risk of post-vaccination complications.

Along with a good anti-allergic effect, they cause a number of side effects. To reduce their risk, treatment is prescribed for 7-10 days. Side effects:

  • dry mucous membranes, thirst;
  • increased heart rate;
  • drop in blood pressure;
  • nausea, vomiting, stomach discomfort;
  • increased appetite.

First generation drugs are not prescribed to people whose activities are associated with increased attention: pilots, drivers, because. they can weaken attention and muscle tone.

Suprastin

Synonyms: Chloropyramine

It is available both in the form of tablets and in ampoules. The active ingredient is chloropyramine. One of the most commonly used antiallergic drugs. Suprastin has a pronounced antihistamine effect. It is prescribed for the treatment of seasonal and chronic rhinitis, urticaria, atopic dermatitis, eczema, Quincke's edema.

Suprastin relieves itching well, including after an insect bite. It is used in the complex therapy of rashes, accompanied by skin itching and scratching. Available in the form of tablets, solutions for injection.

Suprastin is approved for the treatment of infants, starting from one month. The dosage is selected individually depending on the age and body weight of the child. These funds are used in the complex therapy of chicken pox: to relieve skin itching and as a sedative. Suprastin is also included in the lytic mixture ("troychatka"), which is prescribed at a high and not knocked down temperature.

Suprastin is contraindicated for use during pregnancy and breastfeeding.

Tavegil

Synonym: clemastine

It is used in the same cases as suprastin. The drug has a strong antihistamine effect lasting up to 12 hours. Tavegil does not lower blood pressure, the hypnotic effect is less pronounced than that of suprastin. The medicine is available in several forms: tablets and injection.

Application in children. Tavegil has been used since 1 year. The syrup is prescribed for children from 1 year old, tablets can be used from 6 years old. The dosage is determined individually depending on the age and body weight of the child. The dose is selected by the doctor.

Tavegil is prohibited for use during pregnancy.

Synonym: Quifenadine

Fenkarol blocks H-1 histamine receptors and starts an enzyme that utilizes histamine, so the effect of the drug is more stable and long lasting. Fenkarol practically does not cause a sedative and hypnotic effect. In addition, there are indications that this drug has an antiarrhythmic effect. Phencarol is available in the form of tablets and powder for suspension.

Quifenadine (Fenkarol) is used to treat all types of allergic reactions, especially seasonal allergies. This tool is included in the complex treatment of parkinsonism. In surgery, it is used as part of medical preparation for anesthesia (premedication). Fenkarol is used to prevent host-foreign reactions (when the body rejects foreign cells) during transfusions of blood components.

In pediatric practice, the drug is prescribed from 1 year. For children, the suspension is preferable, it has an orange flavor. If the child refuses to take the syrup, a tablet form may be prescribed. The dosage is determined by the doctor, taking into account the weight and age of the child.

Fencarol is contraindicated in the 1st trimester of pregnancy. In the 2nd and 3rd trimester, its use is possible under medical supervision.

Fenistil

Synonym: Dimetinden

The drug is used to treat all types of allergies, skin itching with chickenpox, rubella, prevention of allergic reactions. Fenistil causes drowsiness only at the beginning of treatment. After a few days, the sedative effect disappears. The drug has a number of other side effects: dizziness, muscle spasms, dryness of the oral mucosa.

Fenistil is available in the form of tablets, drops for children, gel and emulsion. Gel and emulsion are applied externally after insect bites, contact dermatitis, sunburn. There is also a cream, but this is a completely different drug based on a different substance and it is used for "cold on the lips".

In children's practice, Fenistil in the form of drops is used from 1 meat. Up to 12 years of age, drops are prescribed, over 12 years of age, capsules are allowed. The gel is used in children from birth. The dosage of drops and capsules is selected by the doctor.

Pregnant women are allowed to use the drug in the form of a gel and drops from 12 weeks of pregnancy. From the second trimester, Fenistil is prescribed only for life-threatening conditions: Quincke's edema and acute food allergies.

Diazolin

Synonym: Mebhydrolin

The drug has low antihistamine activity. Diazolin has a fairly large number of side effects. When it is taken, dizziness, stomach pain, nausea and vomiting, increased heart rate, and frequent urination occur. But at the same time, Diazolin does not cause drowsiness. It is approved for long-term treatment in drivers and pilots.

Available in the form of tablets, powder for suspension and dragee. The duration of antiallergic action is up to 8 hours. It is taken 1-3 times a day.

In children, the drug is prescribed from 2 years of age. Up to 5 years, Diazolin in the form of a suspension is preferable; over 5 years, tablets are allowed. The dosage is selected by the doctor individually.

Diazolin is contraindicated in the first trimester of pregnancy.

Despite all the shortcomings, first-generation drugs are widely used in medical practice. They are well studied, approved for the treatment of young children. Medicines are available in different forms: injection solutions, suspensions, tablets, which makes it convenient to use them and select an individual dosage.

Antihistamines work well for allergic dermatitis, and (in most cases) atopic dermatitis too.

It should be remembered that drugs should be taken in a strictly defined dose, according to the instructions. Otherwise, undesirable effects may occur, even (!) an increase in an allergic reaction.

The choice of medicine and its dose should be performed by a doctor. Antiallergic treatment, especially for children and pregnant women, should be carried out under strict medical supervision.

10 comments

    I have a severe allergy to ragweed (but the list of allergens is not limited to this): itchy eyes, runny nose, sneezing. I started taking levocitemeresin in addition to Avamys (nasal spray). But he does not help me well, because. A strong cough has already begun, especially at night. I didn't sleep at all for one night. Now I don't know what to drink :(

    • There are a lot of drugs, each one is better for something different. Try other drugs from the list, newer.

      Well, it is best to consult a doctor, perhaps you will be prescribed an injectable form.

    Hello! My daughter (16 years old) has frequent recurrences of allergic rhinitis. The last time the doctor prescribed a course of Desal (4 weeks) did not pass and 2 weeks later there was again nasal congestion, fever, and this time severe headaches. Thought it was low blood pressure. When they took the test, it turned out again-allergy. They started taking Desal again. Tell me, is it possible to use antihistamines so often, and what alternative and more effective treatment would you recommend?

    If any one drug from at least the second generation does not help, then you need to try another active ingredient. For example, loratadine does not help my child at all. Doctors automatically prescribe it. :(They used cetrin, drank almost the entire package - everything was fine, as long as the weather was damp and cold. As soon as the sun came out and all the alder-birch trees began to bloom, cetrin does not help. Where the promised effect for three days after the course of treatment is unclear.
    Passed 2 courses of ASIT - so far it has not helped, alas. And drugs for ASIT are very, very expensive.
    Friends say that acupuncture helps. But it is also very expensive. We need to study the issue.

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All information is presented for educational purposes. Do not self-medicate, it is dangerous! An accurate diagnosis can only be made by a doctor.


are substances that inhibit the action of free histamine. When an allergen enters the body, histamine is released from the mast cells of the connective tissue that are part of the body's immune system. It begins to interact with specific receptors and cause itching, swelling, rashes and other allergic manifestations. Antihistamines are responsible for blocking these receptors. There are three generations of these drugs.


1st generation antihistamines

They appeared in 1936 and continue to be used. These drugs reversibly bind to H1 receptors, which explains the need for a large dosage and high frequency of administration.

Antihistamines of the 1st generation are characterized by the following pharmacological properties:

    reduce muscle tone;

    have a sedative, hypnotic and anticholinergic effect;

    potentiate the effects of alcohol;

    have a local anesthetic effect;

    give a quick and strong, but short-term (4-8 hours) therapeutic effect;

    long-term use reduces antihistamine activity, so every 2-3 weeks the funds are changed.

The bulk of 1st generation antihistamines are fat-soluble, can overcome the blood-brain barrier and bind to the H1 receptors of the brain, which explains the sedative effect of these drugs, which is enhanced after taking alcohol or psychotropic drugs. When taking medium therapeutic doses in children and high toxic doses in adults, psychomotor agitation may be observed. Due to the presence of a sedative effect, 1st generation antihistamines are not prescribed to persons whose activities require increased attention.

The anticholinergic properties of these drugs cause atropine-like reactions, such as dryness of the nasopharynx and mouth, urinary retention, visual impairment. These features can be beneficial when, but they can increase airway obstruction caused by bronchial (sputum viscosity increases), exacerbate prostate adenoma, glaucoma and other diseases. At the same time, these drugs have an antiemetic and anti-swaying effect, reduce the manifestation of parkinsonism.

A number of these antihistamines are included in combination products that are used for colds, motion sickness, or that have a sedative or hypnotic effect.

An extensive list of side effects from taking these antihistamines makes them less likely to be used in the treatment of allergic diseases. Many developed countries have banned their implementation.


Diphenhydramine is prescribed for hay, urticaria, sea sickness, air sickness, vasomotor, bronchial asthma, allergic reactions caused by the administration of medicinal substances (for example, antibiotics), in the treatment of peptic ulcer, dermatoses, etc.

    Advantages: high antihistamine activity, reduced severity of allergic, pseudo-allergic reactions. Diphenhydramine has antiemetic and antitussive effects, has a local anesthetic effect, due to which it is an alternative to Novocaine and Lidocaine in case of their intolerance.

    Cons: unpredictability of the consequences of taking the drug, its effects on the central nervous system. It can cause urinary retention and dry mucous membranes. Side effects include sedative and hypnotic effects.

Diazolin

Diazolin has the same indications for use as other antihistamines, but differs from them in the features of the effect.

    Advantages: a mild sedative effect allows it to be used where it is undesirable to have a depressing effect on the central nervous system.

    Cons: irritates the mucous membranes of the gastrointestinal tract, causes dizziness, impaired urination, drowsiness, slows down mental and motor reactions. There is information about the toxic effect of the drug on nerve cells.

Suprastin

Suprastin is prescribed for the treatment of seasonal and chronic allergic conjunctivitis, urticaria, atopic, Quincke's edema, itching of various etiologies,. It is used in parenteral form for acute allergic conditions requiring emergency care.

    Advantages: it does not accumulate in the blood serum, therefore, even with prolonged use it does not cause an overdose. Due to the high antihistamine activity, a rapid therapeutic effect is observed.

    Cons: side effects - drowsiness, dizziness, inhibition of reactions, etc. - are present, although they are less pronounced. The therapeutic effect is short-term, in order to prolong it, Suprastin is combined with H1-blockers that do not have sedative properties.


in the form of injections, it is used for angioedema, as well as anaphylactic shock, as a prophylactic and therapeutic agent for allergic and pseudo-allergic reactions.

    Advantages: It has a longer and stronger antihistamine effect than Diphenhydramine, and has a more moderate sedative effect.

    Cons: can itself cause an allergic reaction, has some inhibitory effect.

Fenkarol

Phencarol is prescribed when addiction to other antihistamines appears.

    Advantages: it has a weak sedative effect, does not have a pronounced inhibitory effect on the central nervous system, has low toxicity, blocks H1 receptors, and is able to reduce the content of histamine in tissues.

    Cons: less antihistamine activity in comparison with Diphenhydramine. Fenkarol is used with caution in the presence of diseases of the gastrointestinal tract, cardiovascular system and liver.

2nd generation antihistamines

They have advantages over first generation drugs:

    there is no sedative and anticholinergic effect, since these drugs do not cross the blood-brain barrier, only some individuals experience moderate drowsiness;

    mental activity, physical activity do not suffer;

    the effect of the drugs reaches 24 hours, so they are taken once a day;

    they are not addictive, which allows them to be prescribed for a long time (3-12 months);

    when you stop taking the drugs, the therapeutic effect lasts about a week;

    drugs are not adsorbed with food in the gastrointestinal tract.

But antihistamines of the 2nd generation have a cardiotoxic effect of varying degrees, therefore, when they are taken, cardiac activity is monitored. They are contraindicated in elderly patients and patients suffering from disorders of the cardiovascular system.

The occurrence of cardiotoxic action is explained by the ability of 2nd generation antihistamines to block the potassium channels of the heart. The risk is increased when these drugs are combined with antifungal drugs, macrolides, antidepressants, grapefruit juice, and if the patient has severe liver dysfunction.

Claridol and Clarisens


used to treat seasonal as well as cyclic allergic rhinitis, allergic, Quincke's edema and a number of other diseases of allergic origin. It copes with pseudo-allergic syndromes and allergies to insect bites. Included in the complex measures for the treatment of itchy dermatoses.

    Benefits: Claridol has antipruritic, antiallergic, antiexudative effects. The drug reduces capillary permeability, prevents the development of edema, relieves spasm of smooth muscles. It does not affect the central nervous system, has no anticholinergic and sedative effect.

    Cons: occasionally after taking Claridol, patients complain of dry mouth, nausea and vomiting.

Clarotadine

Clarotadine contains the active substance loratadine, which is a selective blocker of H1-histamine receptors, on which it has a direct effect, avoiding the undesirable effects inherent in other antihistamines. Indications for use are allergic conjunctivitis, acute chronic and idiopathic urticaria, rhinitis, pseudo-allergic reactions associated with the release of histamine, allergic insect bites, itchy dermatoses.

    Advantages: the drug does not have a sedative effect, is not addictive, acts quickly and for a long time.

    Cons: undesirable consequences of taking Clarodin include disorders of the nervous system: asthenia, anxiety, drowsiness, depression, amnesia, tremor, agitation in a child. Dermatitis may appear on the skin. Frequent and painful urination, constipation and diarrhea. Weight gain due to disruption of the endocrine system. The defeat of the respiratory system can be manifested by cough, bronchospasm, sinusitis and similar manifestations.


indicated for allergic rhinitis (rhinitis) of a seasonal and permanent nature, skin rashes of allergic origin, pseudo-allergies, reactions to insect bites, allergic inflammation of the mucous membrane of the eyeball.

    Benefits: Lomilan is able to relieve itching, reduce the tone of smooth muscles and the production of exudate (a special fluid that appears during the inflammatory process), prevent tissue edema already half an hour after taking the drug. The greatest efficiency comes in 8-12 hours, then subsides. Lomilan is not addictive and does not adversely affect the activity of the nervous system.

    Cons: adverse reactions are rare, manifested by headache, fatigue and drowsiness, inflammation of the gastric mucosa, nausea.

LauraGeksal

    Advantages: the drug has neither anticholinergic nor central action, its intake does not affect the attention, psychomotor functions, working capacity and mental qualities of the patient.

    Cons: LoraGeksal is usually well tolerated, but occasionally it causes fatigue, dry mouth, headache, tachycardia, dizziness, allergic reactions, cough, vomiting, gastritis, liver dysfunction.

Claritin

Claritin contains an active ingredient - loratadine, which blocks H1-histamine receptors and prevents the release of histamine, bradykinin and serotonin. Antihistamine effectiveness lasts a day, and therapeutic comes after 8-12 hours. Claritin is indicated for the treatment of allergic rhinitis, allergic skin reactions, food allergies, and mild asthma.

    Advantages: high efficiency in the treatment of allergic diseases, the drug is not addictive, drowsiness.

    Cons: cases of side effects are rare, they are manifested by nausea, headache, gastritis, agitation, allergic reactions, drowsiness.

Rupafin

Rupafin has a unique active ingredient - rupatadine, which is distinguished by antihistamine activity and a selective effect on H1-histamine peripheral receptors. It is prescribed for chronic idiopathic urticaria and allergic rhinitis.

    Advantages: Rupafin effectively copes with the symptoms of the allergic diseases listed above and does not affect the functioning of the central nervous system.

    Cons: undesirable consequences of taking the drug - asthenia, dizziness, fatigue, headache, drowsiness, dry mouth. It can affect the respiratory, nervous, musculoskeletal, and digestive systems, as well as metabolism and skin.

Zyrtec

Zyrtec is a competitive antagonist of the hydroxyzine metabolite, histamine. The drug facilitates the course and sometimes prevents the development of allergic reactions. Zyrtec limits the release of mediators, reduces the migration of eosinophils, basophils, neutrophils. The drug is used for allergic rhinitis, bronchial asthma, urticaria, conjunctivitis, dermatitis, fever, skin, angioedema.

    Benefits: effectively prevents the occurrence of edema, reduces capillary permeability, relieves smooth muscle spasm. Zyrtec does not have anticholinergic and antiserotonin effects.

    Cons: improper use of the drug can lead to migraines, drowsiness, allergic reactions.


blocks histamine receptors that increase vascular permeability, causing muscle spasms, leading to an allergic reaction. It is used to treat allergic conjunctivitis, rhinitis and chronic idiopathic urticaria.

    Advantages: the drug acts an hour after application, the therapeutic effect lasts for 2 days. A five-day intake of Kestin allows you to maintain an antihistamine effect for about 6 days. Sedative effects are practically non-existent.

    Cons: the use of Kestin can cause insomnia, abdominal pain, nausea, drowsiness, asthenia, headache, sinusitis, dry mouth.

New antihistamines, 3rd generation


These substances are prodrugs, which means that when they enter the body, they are converted from their original form into pharmacologically active metabolites.

All 3rd generation antihistamines do not have a cardiotoxic and sedative effect, so they can be used by people whose activities are associated with a high concentration of attention.

These drugs block H1 receptors, and also have an additional effect on allergic manifestations. They have high selectivity, do not overcome the blood-brain barrier, therefore they are not characterized by negative effects from the central nervous system, there is no side effect on.

The presence of additional effects contributes to the use of 3rd generation antihistamines in the long-term treatment of most allergic manifestations.


is prescribed as a therapeutic and prophylactic agent for hay fever, allergic skin reactions, including urticaria, allergic rhinitis. The effect of the drug develops within 24 hours and reaches a maximum after 9-12 days. Its duration depends on the previous therapy.

    Advantages: the drug has practically no sedative effect, does not enhance the effect of taking sleeping pills or alcohol. It also does not affect the ability to drive a car or mental activity.

    Cons: Gismanal can cause increased appetite, dry mucous membranes, tachycardia, drowsiness, QT prolongation, palpitations, collapse.


is a fast-acting selectively active H1 receptor antagonist, a derivative of butyrophenone, which differs in chemical structure from analogues. It is used in allergic rhinitis to relieve its symptoms, allergic dermatological manifestations (dermographism, contact dermatitis, urticaria, atonic eczema,), asthma, atonic and provoked by exercise, as well as in connection with acute allergic reactions to various irritants.

    Benefits: no sedative and anticholinergic effect, no effect on psychomotor activity and well-being of a person. The drug is safe to use in patients with glaucoma and prostate disorders.


- a highly effective antihistamine drug, which is a metabolite of terfenadine, therefore, has a great similarity with histamine H1 receptors. Telfast binds to them and blocks them, preventing their biological manifestations as allergic symptoms. Mast cell membranes are stabilized and the release of histamine from them is reduced. Indications for use are angioedema, urticaria, hay fever.

    Advantages: does not show sedative properties, does not affect the speed of reactions and concentration of attention, heart function, is not addictive, highly effective against the symptoms and causes of allergic diseases.

    Cons: rare consequences of taking the drug are headache, nausea, dizziness, very rarely there is shortness of breath, anaphylactic reaction, skin flushing.


The drug is used to treat seasonal allergic rhinitis with the following manifestations of hay fever: skin itching, sneezing, rhinitis, redness of the mucous membrane of the eyes, as well as for the treatment of chronic idiopathic urticaria and its symptoms: skin itching, redness.

    Advantages- when taking the drug, side effects characteristic of antihistamines do not appear: visual impairment, constipation, dryness of the oral mucosa, weight gain, a negative effect on the functioning of the heart muscle. The drug can be purchased at a pharmacy without a prescription, no dose adjustment is required for the elderly, patients and renal and hepatic insufficiency. The drug acts quickly, maintaining its effect during the day. The price of the drug is not too high, it is available to many people suffering from.

    Flaws- after some time, addiction to the action of the drug is possible, it has side effects: dyspepsia, dysmenorrhea, tachycardia, headache and dizziness, anaphylactic reactions, taste perversion. Dependence on the drug may form.


The drug is prescribed for the appearance of seasonal allergic rhinitis, as well as for chronic.

    Advantages- the drug is rapidly absorbed, reaching the desired one within an hour after ingestion, this action continues throughout the day. Its reception does not require restrictions for people operating complex mechanisms, driving vehicles, and does not cause a sedative effect. Fexofast is available without a prescription, has an affordable price, and is highly effective.

    Flaws- for some patients, the drug brings only temporary relief, without bringing a complete recovery from the manifestations of allergies. It has side effects: swelling, increased drowsiness, nervousness, insomnia, weakness, increased allergy symptoms in the form of itching, skin rash.


The drug is prescribed for the symptomatic treatment of hay fever (pollinosis), urticaria, allergic and allergic conjunctivitis with itching, lacrimation, conjunctival hyperemia, dermatosis with rash and rashes, angioedema.

    Advantages– Levocitirizine-Teva quickly shows its effectiveness (after 12-60 minutes) and during the day it prevents the appearance and weakens the course of allergic reactions. The drug is rapidly absorbed, showing 100% bioavailability. It can be used for long-term treatment and for emergency help with seasonal exacerbations of allergies. Available for the treatment of children from 6 years.

    Flaws- has such side effects as drowsiness, irritability, nausea, headache, weight gain, tachycardia, abdominal pain, migraine. The price of the medicine is quite high.


The drug is used for the symptomatic treatment of such manifestations of pollinosis and urticaria as skin itching, sneezing, inflammation of the conjunctiva, rhinorrhea, Quincke's edema, allergic dermatoses.

    Advantages– Ksizal has a pronounced anti-allergic orientation, being a very effective remedy. It prevents the onset of allergy symptoms, facilitates their course, and has no sedative effect. The drug acts very quickly, maintaining its effect for a day from the moment of administration. Ksizal can be used to treat children from 2 years of age, it is available in two dosage forms (tablets, drops) that are acceptable for use in pediatrics. It eliminates nasal congestion, the symptoms of chronic allergies are quickly stopped, it does not have a toxic effect on the heart and central nervous system.

    Flaws- the remedy may exhibit the following side effects: dry mouth, fatigue, abdominal pain, pruritus, hallucinations, shortness of breath, convulsions, muscle pain.


The drug is indicated for the treatment of seasonal hay fever, allergic rhinitis, chronic idiopathic urticaria with symptoms such as lacrimation, cough, itching, swelling of the nasopharyngeal mucosa.

    Advantages- Erius acts exceptionally quickly on allergy symptoms, can be used to treat children from one year old, as it has a high degree of safety. Well tolerated by both adults and children, it is available in several dosage forms (tablets, syrup), which is very convenient for use in pediatrics. It can be taken for a long time period (up to a year) without causing addiction (resistance to it). Reliably stops the manifestations of the initial phase of the allergic response. After a course of treatment, the effect of it persists for 10-14 days. Overdose symptoms were not observed even with a fivefold increase in the dose of Erius.

    Flaws- side effects may occur (nausea and headache, tachycardia, local allergic symptoms, diarrhea, hyperthermia). Children usually have insomnia, headache, fever.


The drug is intended for the treatment of allergic manifestations such as allergic rhinitis, and urticaria, marked by itching and skin rashes. The drug stops such symptoms of allergic rhinitis as sneezing, itching in the nose and in the sky, watery eyes.

    Advantages– Desal prevents the appearance of edema, muscle spasm, reduces capillary permeability. The effect of taking the drug can be seen after 20 minutes, it lasts for a day. A single dose of the medicine is very convenient, two forms of its release are syrup and tablets, the intake of which does not depend on food. Since Desal is taken to treat children from 12 months of age, the syrup form of the drug is in demand. The drug is so safe that even a 9-fold excess of the dose does not lead to negative symptoms.

    Flaws- occasionally, symptoms of side effects such as increased fatigue, headache, dryness of the oral mucosa may occur. Additionally, side effects such as insomnia, tachycardia, the appearance of hallucinations, diarrhea, and hyperactivity are manifested. Allergic manifestations of side effects are possible: itching, urticaria, angioedema.

4th generation antihistamines - do they exist?

All statements by advertisers positioning drug brands as “fourth-generation antihistamines” are nothing more than a publicity stunt. This pharmacological group does not exist, although marketers include not only newly created drugs, but also second-generation drugs.

The official classification indicates only two groups of antihistamines - these are first and second generation drugs. The third group of pharmacologically active metabolites is positioned in pharmaceuticals as "H 1 histamine blockers of the third generation."



For the treatment of allergic manifestations in children, antihistamines of all three generations are used.

Antihistamines of the 1st generation are distinguished by the fact that they quickly show their healing properties and are excreted from the body. They are in demand for the treatment of acute manifestations of allergic reactions. They are prescribed in short courses. The most effective of this group is Tavegil, Suprastin, Diazolin, Fenkarol.

A significant percentage of side effects leads to a reduction in the use of these drugs for childhood allergies.

Antihistamines of the 2nd generation do not cause sedation, act for a longer time and are usually used once a day. Few side effects. Among the drugs in this group, Ketotifen, Fenistil, Cetrin are used to treat manifestations of childhood allergies.

3rd generation antihistamines for children include Gismanal, Terfen and others. They are used in chronic allergic processes, since they are able to stay in the body for a long time. There are no side effects.

Erius can be attributed to newer drugs.

Negative consequences:

    1st generation: headache, constipation, tachycardia, drowsiness, dry mouth, blurred vision, urinary retention and lack of appetite;

    2nd generation: negative effect on the heart and;

For children, antihistamines are produced in the form of ointments (allergic reactions on the skin), drops, syrups and tablets for oral administration.

Antihistamines during pregnancy


In the first trimester of pregnancy, it is forbidden to take antihistamines. In the second, they are prescribed only in extreme cases, since none of these remedies is absolutely safe.

Natural antihistamines, which include vitamins C, B12, pantothenic, oleic and nicotinic acids, zinc, fish oil, can help get rid of some allergic symptoms.

The safest antihistamines are Claritin, Zirtek, Telfast, Avil, but their use must be agreed with the doctor without fail.

4 Best Natural Antihistamines

In some cases, you can resort to the help of the following funds, which can suppress the production of histamine in the body.

    Quercetin. Quercetin is an antioxidant known for its anti-inflammatory properties. It is found in some foods, such as onions and apples. Scientists became interested in the ability of quercetin to reduce the severity of an allergic reaction. The experiment was carried out on rats. Based on its results, it was concluded that quercetin is able to reduce the intensity of the allergic and inflammatory process in the respiratory system. People with allergies can either purchase quercetin in supplements or just eat foods that are rich in this antioxidant.

    Bromelain. Bromelain is an enzyme found in high amounts in pineapples. There is evidence that it helps to reduce the intensity of allergy symptoms. To have a positive effect, it is recommended to take 400-500 mg of this substance 3 times a day. Alternatively, you can simply enrich your diet with pineapples, which hold the record for the content of this substance.

    Vitamin C. Vitamin C is found in various foods. This antioxidant has properties to suppress the symptoms of an allergic reaction. Vitamin C is non-toxic, its intake in moderate dosages does not harm the human body. Therefore, it can be safely used as an antihistamine. The recommended dose of vitamin C for allergy sufferers is 2 g. This amount is found in 3-5 citrus fruits. They need to be eaten throughout the day.

Food to help fight allergies

To cope with allergies, it is not necessary to empty the pharmacy shelves. Sometimes it is enough to minimize contact with the allergen and enrich your menu with products that have antihistamine properties. A proper diet, combined with physical activity, will help the immune system resist attacks from the external environment.

As for antioxidants in the form of supplements, they should be taken only after consultation with a specialist. The best way to get these substances is from food. So they will be absorbed by 100%.


    Natural Treatment of Perennial Allergic Rhinitis
    http://www.altmedrev.com/archive/publications/5/5/448.pdf

    Quercetin inhibits transcriptional up-regulation of histamine H1 receptor via suppressing protein kinase C-?/extracellular signal-regulated kinase/poly(ADP-ribose) polymerase-1 signaling pathway in HeLa cells
    https://www.ncbi.nlm.nih.gov/pubmed/23333628

    Anti-inflammatory activity of quercetin and isoquercitrin in experimental murine allergic asthma
    https://www.ncbi.nlm.nih.gov/pubmed/18026696


About the doctor: From 2010 to 2016 practicing physician of the therapeutic hospital of the central medical unit No. 21, the city of Elektrostal. Since 2016, she has been working at the diagnostic center No. 3.